- Synthesis method of 2-chloro-4,6-dimethoxypyrimidine
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The invention provides a synthesis method of 2-chloro-4,6-dimethoxypyrimidine and belongs to the technical field of organic synthesis. A synthesis route that malononitrile, methanol, acetyl chloride,hydrogen cyanamide and alkali liquor are taken as raw materials is adopted, malononitrile is dropwise added into a system of malononitrile and methanol, 1,3-dimethamidine dihydrochloride is directly obtained, then reaction is carried out with sodium bicarbonate and hydrogen cyanamide to obtain 3-amino-3-methoxy-N-nitrile-2-propyl amidine, and further reaction is carried out with hydrogen chloride,so that 2-chloro-4,6-dimethoxypyrimidine is obtained. The synthesis method provided by the invention has the advantages that tedious synthesis process and equipment of 1,3-dimethamidine dihydrochloride are eliminated, acetyl chloride is added into the malononitrile and methanol, and 1,3-dimethamidine dihydrochloride is directly obtained by virtue of a one-step method. The synthesis route of 1,3-dimethamidine dihydrochloride has the advantages that moisture is controlled to be extremely low, product quality is stable and yield is high.
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Paragraph 0014; 0020; 0025; 0026; 0027; 0028; 0033; 0034
(2018/03/23)
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- Substituted Pyrrolidines and Methods of Use
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The invention discloses compounds of Formula (I) wherein R1, R2, R2A, R3, R3A, R4, and R5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
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Paragraph 1583; 1594
(2018/04/20)
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- Dimethoxypyrimidines as Novel Herbicides. Part 1. Synthesis and Herbicidal Activity of Dimethoxyphenoxypyrimidines and Analogues
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A number of 6-(4-phenoxyphenoxy)pyrimidines and triazines were synthesized and their herbicidal activity was measured. Compounds with the methoxy groups at the 2- and 4-positions on the pyrimidine and triazine rings exhibited high herbicidal activity. Introduction of a substituent into the 5-position of the pyrimidine ring diminished the activity. In the phenoxyphenoxy substructure at the 6-position, the central ether bond can be replaced by a methylene group without loss of activity. The optimum substituent on the terminal phenyl ring was 3-trifluoromethyl. The compounds showed a strong Hill reaction inhibition, but unfortunately showed poor selectivity between weeds and crops. - Keywords: phenoxyphenoxypyrimidines; phenoxyphenoxy-s-triazines; Hill reaction inhibitors; 2,6-dimethoxy-4-pyrimidine; 2,6-dimethoxy-4--s-triazine; herbicides
- Nezu, Yukio,Miyazaki, Masahiro,Sugiyama, Kazuhiko,Kajiwara, Ikuo
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p. 103 - 114
(2007/10/03)
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- Process for the production of 2-halo-4,6-dialkoxy pyrimidines
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A process for the production of 2-halo-4,6-dialkoxypyrimidines of the general formula: STR1 starting from a propanediimidate or its salts. In the first stage, a propanediimidate or its salts of the general formula: STR2 is/are converted with cyanamide of the formula: in the presence of a base at a pH values above pH 7 into a cyanimidate of the general formula: STR3 The latter is then converted in the second stage with a hydrogen halide into the end product according to formula I.
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- 2-(4,6-dimethoxy-2-pyrimidinyloxy)benzaldoximes, preparation processes thereof, herbicides containing the same, and herbicidal compositions containing the same along with other active ingredient
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Disclosed are herbicidally active pyrimidine derivatives of the formula STR1 wherein R represents a hydrogen atom or an etherifying group, e.g., a lower alkyl, lower alkenyl, lower alkynyl, phenyl-substituted lower alkenyl, lower haloalkenyl, cycloalkyl, substituted phenyl-substituted lower alkenyl or phenyl-substituted lower alkynyl group; or a group represented by the following formula: STR2 wherein R1 represents a hydrogen atom or a lower alkyl group, X a halogen atom or a lower alkyl or lower alkoxyl group, m and n individually 0-2, and when m is 2, both Xs may be the same or different, and herbicidal compositions containing the same, alone or in combination with another herbicidally active compound, the pyrimidine derivatives being prepared by reaction of 2-(4,6-dimethoxy-2-pyrimidinyloxy)benzaldehyde with NH2 OR or with a salt of hydroxylamine followed by reaction with a halide of the formula RY wherein R has the same value as above and Y is Cl, Br or I.
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